IspC from P. falciparum

[75] Behrendt C. T., Kunfermann A., Illarionova V., Matheeussen A., Pein M. K., Gräwert T., Kaiser J., Bacher A., Eisenreich W., Illarionov B., Fischer M., Maes L., Groll M., Kurz T.
Reverse fosmidomycin derivatives against the antimalarial drug target IspC (Dxr)
J. Med. Chem., 2011, 54, 6796-802, PDF

Reverse hydroxamate-based inhibitors of IspC, a key enzyme of the non-mevalonate pathway of isoprenoid biosynthesis and a validated antimalarial target, were synthesized and biologically evaluated. The binding mode of one derivative in complex with EcIspC and a divalent metal ion was clarified by X-ray analysis. Pilot experiments have demonstrated in vivo potential.